Rosuvastatin calcium 40 mg
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Rosuvastatin Calcium 40 mg: Efficacy, Stability, and Clinical Applications
Introduction to Rosuvastatin Calcium 40 mg
Rosuvastatin calcium, commonly known by its brand name Crestor, is a potent statin used to lower cholesterol levels, particularly low-density lipoprotein cholesterol (LDL-C). The 40 mg dosage is often prescribed for patients with severe hypercholesterolemia or those at high risk of cardiovascular events. This article synthesizes recent research on the formulation, efficacy, safety, and pharmacokinetics of rosuvastatin calcium 40 mg.
Formulation and Stability of Rosuvastatin Calcium Tablets
Stabilization with Tribasic Calcium Phosphate
Rosuvastatin calcium is known to be unstable during storage. Recent advancements have led to the development of a directly compressible immediate-release tablet formulation stabilized with tribasic calcium phosphate. This formulation ensures good mechanical properties, rapid disintegration, and a fast dissolution rate, with 85% of the drug substance dissolving within 15 minutes. Additionally, the tablets exhibit satisfactory chemical stability under stress conditions, outperforming some commercial products1.
Process Validation and Quality Assurance
The manufacturing process for rosuvastatin calcium 40 mg tablets involves a wet granulation method, which has been validated to ensure consistent product quality. Key quality attributes such as blend uniformity, compression assay, hardness, thickness, disintegration, and dissolution have been found to be within acceptable limits. The tablets have also demonstrated bioequivalence with the reference listed drug (RLD), Codine®, in both fasting and fed states2.
Efficacy of Rosuvastatin Calcium 40 mg
Superior LDL-C Reduction
Rosuvastatin calcium 40 mg has shown superior efficacy in reducing LDL-C levels compared to other statins such as atorvastatin, simvastatin, and pravastatin. In the STELLAR trial, a significant proportion of patients achieved LDL-C levels below 100 mg/dL with rosuvastatin compared to other statins. This efficacy extends to high-risk patients, with more achieving LDL-C goals according to various international guidelines3 4.
Comparison with Atorvastatin
The POLARIS study compared rosuvastatin 40 mg with atorvastatin 80 mg in high-risk patients. Rosuvastatin 40 mg resulted in a greater reduction in LDL-C levels and a higher percentage of patients achieving LDL-C goals. Additionally, rosuvastatin showed significant improvements in high-density lipoprotein cholesterol (HDL-C) and apolipoprotein A-I levels, indicating a more favorable lipid profile5.
Combination Therapy with Ezetimibe
For patients who do not achieve LDL-C goals on statin monotherapy, combination therapy with ezetimibe has been investigated. The EXPLORER study found that combining rosuvastatin 40 mg with ezetimibe 10 mg significantly improved LDL-C reduction and goal achievement compared to rosuvastatin alone. This combination therapy also enhanced other lipid parameters, making it a viable option for high-risk patients7.
Safety and Pharmacokinetics
Endothelial Protection
Rosuvastatin 40 mg has been shown to prevent endothelial dysfunction induced by ischemia and reperfusion (IR) through a cyclooxygenase-2 (COX-2)-dependent mechanism. This protective effect highlights the potential cardiovascular benefits of rosuvastatin beyond lipid-lowering6.
Drug-Drug Interactions
A study on the pharmacokinetic interactions between rosuvastatin, telmisartan, and amlodipine revealed that coadministration increases the pharmacokinetic exposure of rosuvastatin and telmisartan, but not amlodipine. Despite these interactions, the changes were not deemed clinically significant, and all treatments were well-tolerated8.
Conclusion
Rosuvastatin calcium 40 mg is a highly effective statin for lowering LDL-C levels and achieving lipid goals, particularly in high-risk patients. Advances in tablet formulation have improved its stability and bioavailability, while clinical studies have confirmed its superior efficacy and safety profile. Combination therapies and its protective effects on endothelial function further enhance its clinical utility.
Sources and full results
Most relevant research papers on this topic
Directly compressible formulation of immediate release rosuvastatin calcium tablets stabilized with tribasic calcium phosphate
Rosuvastatin calcium tablets stabilized with tribasic calcium phosphate exhibit good mechanical properties, rapid disintegration, and fast dissolution, with satisfactory chemical stability during storage at 50°C/80% RH.
Process validation and in vitro-in vivo evaluation of rosuvastatin calcium tablets
The wet granulation process for manufacturing rosuvastatin calcium tablets 40 mg consistently meets pre-determined specifications and quality attributes, providing high assurance for consistent product quality.
Rosuvastatin is Cost-Effective in Treating Patients to Low-Density Lipoprotein-Cholesterol Goals Compared with Atorvastatin, Pravastatin and Simvastatin: Analysis of the Stellar Trial
Rosuvastatin is a cost-effective statin option for achieving LDL-C goals in patients with hypercholesterolaemia compared to atorvastatin, pravastatin, and simvastatin.
Observational StudyComparison of the efficacy of rosuvastatin versus atorvastatin, simvastatin, and pravastatin in achieving lipid goals: results from the STELLAR trial
Rosuvastatin is more effective than atorvastatin, simvastatin, and pravastatin in achieving lipid goals for patients with high risk of coronary heart disease.
RCT
Large Human Trial
Highly CitedEfficacy and safety of rosuvastatin 40 mg versus atorvastatin 80 mg in high-risk patients with hypercholesterolemia: results of the POLARIS study.
Rosuvastatin 40 mg/day provides greater LDL-C-lowering efficacy than atorvastatin 80 mg/day, enabling more patients to achieve LDL-C goals in high-risk patients with hypercholesterolemia.
RCTLarge Human TrialHighly CitedRosuvastatin prevents conduit artery endothelial dysfunction induced by ischemia and reperfusion by a cyclooxygenase-2-dependent mechanism.
Rosuvastatin prevents ischemia and reperfusion-induced conduit artery endothelial dysfunction through a COX-2-dependent mechanism.
RCTEfficacy and safety of rosuvastatin 40 mg alone or in combination with ezetimibe in patients at high risk of cardiovascular disease (results from the EXPLORER study).
Rosuvastatin 40 mg combined with ezetimibe 10 mg significantly improves LDL cholesterol goals in high-risk patients compared to statin monotherapy.
RCTLarge Human TrialHighly CitedPharmacokinetic Interaction Between Rosuvastatin, Telmisartan, and Amlodipine in Healthy Male Korean Subjects: A Randomized, Open-label, Multiple-dose, 2-period Crossover Study.
Pharmacokinetic interactions between rosuvastatin, telmisartan, and amlodipine are similar in healthy male Korean subjects, with no significant differences in adverse events.
RCTComparison of short-term renal effects and efficacy of rosuvastatin 40 mg and simvastatin 80 mg, followed by assessment of long-term renal effects of rosuvastatin 40 mg, in patients with dyslipidemia.
Rosuvastatin 40 mg effectively lowers cholesterol levels and helps more patients achieve LDL-C goals, with minimal long-term renal effects.
RCTLarge Human TrialLong-term efficacy and safety of rosuvastatin 40 mg in patients with severe hypercholesterolemia.
Long-term treatment with rosuvastatin 40 mg is safe and effective in patients with severe hypercholesterolemia, reducing LDL cholesterol and increasing HDL cholesterol.
Non-RCTLarge Human Trial